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化学工业与工程 2014, Vol. 31 Issue (4) :46-51    DOI: doi: 10.13353/j.issn.1004.9533.2014.04.010
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正交设计优化尼美舒利NLC处方组成与制备工艺
杜广盛1,2, 李德馨2, 魏振平1
(1.天津大学化工学院,天津 300072;2.天津天士力集团化学药物研究所,天津 300410)
Optimization of Formulation and Preparation Parameters for Nimesulide Loaded NLC by Orthogonal Design
 DU  Guang-Sheng1,2, LI  De-Xin2, WEI  Zhen-Ping1
(1. School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; 2. Chemical Pharm R&D Institute, Tianjin Tasly group, Tianjin 300410, China)

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摘要 运用高压均质法制备了加载尼美舒利的纳米结构脂质载体(Nanostructured Lipid Nanoparticles, NLC),采用单因素设计考察了固液态油脂比、脂质用量、乳化剂用量、药脂比、均质压力和均质次数对纳米粒质量的影响。采用正交设计优化了制备条件。确定的最适宜制备方案为油酸与单硬脂酸甘油酯(glycerin monostearate,GMS)投料比为3:10,药脂比为1:40, TPGS用量为1.4 g,均质压力为90 MPa。依据最适宜处方制备的纳米粒粒径为132.6± 1.4 nm,包封率为82.35±1.23%。扫描电镜显示所制备纳米粒呈类球形,体外释放实验表明其释放行为符合Higuchi模型。
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杜广盛
李德馨
魏振平
关键词正交设计;   NLC;   高压均质法;   尼美舒利;   优化     
Abstract: High pressure homogenization method was used to prepare Nimesulide loaded nanostructured lipid nanoparticles (NLC). Single factor design was chosen to study the influence of solid-liquid lipid ratio, amount of lipid, amount of emulsifier, drug-lipid ratio, homogenization pressure and homogenization cycles on quality of the prepared nanoparticles. Orthogonal design was used to optimize the preparation parameters. The optimal preparation method was 3:10 of oleic acid glycerin monostearate(GMS) ratio, 1:40 of drug-lipid ratio, 1.4 g of TPGS, 90 MPa of homogenization pressure. Particle size and entrapment efficiency of NLC prepared by optimal conditions were 132.6±1.4 nm and 82.35±1.23%, respectively. The scanning electron microscope showed that the nanoparticles were of spherical shape. The in vitro release study showed that release behavior accorded with Higuchi model.
Keywordsorthogonal design;   nanostructured lipid nanoparticles (NLC);   homogenization method;   Nimesulide;   optimization     
Received 2013-05-20;
Corresponding Authors: 李德馨,电话:(022)26736518。      Email: lisa@tasly.com
About author: 杜广盛(1988-),男,硕士研究生,主要从事药物新技术与新剂型研究。
引用本文:   
杜广盛, 李德馨, 魏振平.正交设计优化尼美舒利NLC处方组成与制备工艺[J].  化学工业与工程, 2014,31(4): 46-51
DU Guang-Sheng, LI De-Xin, WEI Zhen-Ping.Optimization of Formulation and Preparation Parameters for Nimesulide Loaded NLC by Orthogonal Design[J].  Chemcial Industry and Engineering, 2014,31(4): 46-51
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